methyl di((11Z,14Z)-icosa-11,14-dienyl)amine | 1443413-74-8

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: methyl di((11Z,14Z)-icosa-11,14-dienyl)amine
• 英文别名: (11Z,14Z)-N-[(11Z,14Z)-icosa-11,14-dienyl]-N-methylicosa-11,14-dien-1-amine
• CAS: 1443413-74-8
• 化学式: C₄₁H₇₇N
• 分子量: 584.069
• InChiKey: GOSFVAANLNDKBK-QYCRHRGJSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  16.9
• 重原子数：
  42
• 可旋转键数：
  34
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.8
• 拓扑面积：
  3.2
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为产物：
  描述：

  甲胺 、 (11Z,14Z)-icosa-11,14-dienyl methanesulfonate 以Compound II-3 (1.27 g, 54.4%) was obtained in the same manner as that in Referential Example 1的产率得到methyl di((11Z,14Z)-icosa-11,14-dienyl)amine
  参考文献：
  名称：

  RNAi PHARMACEUTICAL COMPOSITION FOR SUPPRESSING EXPRESSION OF KRAS GENE

  摘要：

  本发明提供了一种抑制KRAS基因表达的组合物，包括含有脂质粒的药物，该药物为具有反义链的双链核酸，其具有与序列编号为1至3的任一KRAS基因mRNA的至少19个连续碱基序列互补的碱基序列；以及由以下式子（I）表示的阳离子脂质： 其中R1和R2相同或不同，均为具有12至24个碳原子的线性或支链烷基，烯基或炔基；L1和L2相同或不同，均为—CO—O—或—O—CO—；a和b相同或不同，均为1至3；R3为氢原子，具有1至6个碳原子的烷基或具有3至6个碳原子的烯基等。

  公开号：

  US20140044755A1

文献信息

• LIPID NANO PARTICLES COMPRISING COMBINATION OF CATIONIC LIPID
  申请人：KYOWA HAKKO KIRIN CO., LTD.

  公开号：US20140045913A1

  公开（公告）日：2014-02-13

  The present invention provides a lipid nano-particles, which allow nucleic acids to be easily introduced into cells, comprising a cationic lipid represented by formula (I) (wherein: R 1 and R 2 are, the same or different, alkenyl, etc, and X 3 is absent or is alkyl, etc, X 1 and X 2 are hydrogen atoms, or are combined together to form a single bond or alkylene, and Y 1 is absent or anion, L 1 is a single bond, etc, R 3 is alkyl, etc), and a cationic lipid represented by formula (II) (wherein: R 4 and R 5 are, the same or different, alkenyl, etc, and X 4 and X 5 are hydrogen atoms, or are combined together to form a single bond or alkylene, and X 6 is absent or is alkyl, etc, Y 2 is absent or anion, a and b are, the same or different, 0 to 3, and L 4 is a single bond, etc, R 6 is alkyl, etc, L 2 and L 3 are —O—, —CO—O— or —O—CO—), and the like.

  本发明提供了一种脂质纳米粒子，可以使核酸轻松地进入细胞，包括由式(I)表示的阳离子脂质（其中：R1和R2是相同或不同的烯基等，X3不存在或是烷基等，X1和X2是氢原子，或结合在一起形成单键或亚烷基，Y1不存在或是阴离子，L1是单键等，R3是烷基等），以及由式(II)表示的阳离子脂质（其中：R4和R5是相同或不同的烯基等，X4和X5是氢原子，或结合在一起形成单键或亚烷基，X6不存在或是烷基等，Y2不存在或是阴离子，a和b是相同或不同的0到3，L4是单键等，R6是烷基等，L2和L3是—O—，—CO—O—或—O—CO—）等。
• LIPID NANO PARTICLES COMPRISING CATIONIC LIPID FOR DRUG DELIVERY SYSTEM
  申请人：Kyowa Hakko Kirin Co., Ltd.

  公开号：US20140039032A1

  公开（公告）日：2014-02-06

  The present invention provides a lipid nano-particles, which allow nucleic acids to be easily introduced into cells, comprising a cationic lipid represented by formula (I) (wherein: R 1 and R 2 are, the same or different, alkenyl, etc, and X 3 is absent or is alkyl, etc, X 1 and X 2 are hydrogen atoms, or are combined together to form a single bond or alkylene, and Y 1 is absent or anion, L 1 is a single bond, etc, R 3 is alkyl, etc), and the like.

  本发明提供了一种脂质纳米粒子，允许核酸轻松地被引入细胞中，包括由式(I)表示的阳离子脂质（其中：R1和R2是相同或不同的烯基等，X3不存在或是烷基等，X1和X2是氢原子，或结合在一起形成单键或亚烷基，Y1不存在或是阴离子，L1是单键等，R3是烷基等），等等。
• LIPID NANOPARTICLES FOR DRUG DELIVERY SYSTEM CONTAINING CATIONIC LIPIDS
  申请人：Kyowa Hakko Kirin Co., Ltd.

  公开号：EP2792367A1

  公开（公告）日：2014-10-22

  The present invention provides a lipid nano-particles, which allow nucleic acids to be easily introduced into cells, comprising a cationic lipid represented by formula (I) (wherein: R1 and R2 are, the same or different, alkenyl, etc, and X3 is absent or is alkyl, etc, X1 and X2 are hydrogen atoms, or are combined together to form a single bond or alkylene, and Y1 is absent or anion, L1 is a single bond, etc, R3 is alkyl, etc), and the like.

  本发明提供了一种可将核酸轻松导入细胞的脂质纳米颗粒，它由式(I)代表的阳离子脂质组成 其中R1 和 R2 是相同或不同的烯基等，以及 X3 不存在或为烷基等、 X1 和 X2 为氢原子，或结合在一起形成单键或亚烷基，以及 Y1 不存在或为阴离子、 L1 是单键等、 R3为烷基等）等。
• LIPID NANOPARTICLES CONTAINING COMBINATIONS OF CATIONIC LIPIDS
  申请人：Kyowa Hakko Kirin Co., Ltd.

  公开号：EP2792368A1

  公开（公告）日：2014-10-22

  The present invention provides a lipid nano-particles, which allow nucleic acids to be easily introduced into cells, comprising a cationic lipid represented by formula (I) (wherein: R1 and R2 are, the same or different, alkenyl, etc, and X3 is absent or is alkyl, etc, X1 and X2 are hydrogen atoms, or are combined together to form a single bond or alkylene, and Y1 is absent or anion, L1 is a single bond, etc, R3 is alkyl, etc), and a cationic lipid represented by formula (II) (wherein: R9 and R5 are, the same or different, alkenyl, etc, and X4 and X5 are hydrogen atoms, or are combined together to form a single bond or alkylene, and X6 is absent or is alkyl, etc, Y2 is absent or anion, a and b are, the same or different, 0 to 3, and L9 is a single bond, etc, R6 is alkyl, etc, L2 and L3 are -O-, -CO-O- or -O-CO-), and the like.

  本发明提供了一种可将核酸轻松导入细胞的脂质纳米颗粒，它包括 由式(I)表示的阳离子脂质 其中R1和R2是相同或不同的烯基等，X3不存在或为烷基等、 X1 和 X2 为氢原子，或结合在一起形成单键或亚烷基，以及 Y1 不存在或为阴离子、 L1 是单键等、 R3 是烷基等），以及 由式（II）代表的阳离子脂质 (其中：R9 和 R5 是相同或不同的烯基等，以及 X4 和 X5 为氢原子，或结合在一起形成单键或亚烷基，以及 X6 不存在或为烷基等、 Y2 不存在或为阴离子、 a 和 b 相同或不同，0 至 3，以及 L9 是单键等、 R6 为烷基等 L2和L3为-O-、-CO-O-或-O-CO-）等。
• RNAI PHARMACEUTICAL COMPOSITION CAPABLE OF SUPPRESSING EXPRESSION OF KRAS GENE
  申请人：Kyowa Hakko Kirin Co., Ltd.

  公开号：EP2873732A1

  公开（公告）日：2015-05-20

  The present invention provides a composition for suppressing the expression of a KRAS gene, comprising a lipid particle containing, as a drug, a double-stranded nucleic acid having an antisense strand having a sequence of bases complementary to the sequence of at least 19 continuous bases of any one KRAS gene's mRNA of sequence Nos. 1 to 3; and a cationic lipid represented by the following formula (I): wherein R1 and R2, which are the same or different, are each linear or branched alkyl, alkenyl or alkynyl having a carbon number of from 12 to 24; L1 and L2, which are the same or different, are each -CO-O- or -O-CO-; a and b, which are the same or different, are each 1 to 3; and R3 is a hydrogen atom, alkyl having a carbon number of from 1 to 6, or alkenyl having a carbon number of from 3 to 6, and the like.

  本发明提供了一种用于抑制 KRAS 基因表达的组合物，该组合物包括一种脂质颗粒，其中含有作为药物的双链核酸，该双链核酸具有反义链，该反义链的碱基序列与序列号为 1 至 3 的任一种 KRAS 基因 mRNA 的至少 19 个连续碱基序列互补；以及 由下式（I）代表的阳离子脂质： 其中 R1 和 R2（相同或不同）各自为直链或支链烷基、烯基或炔基，其碳原子数为 12 至 24； 相同或不同的 L1 和 L2 各为-CO-O-或-O-CO-； 相同或不同的 a 和 b 各为 1 至 3；以及 R3 是氢原子、碳原子数为 1-6 的烷基或碳原子数为 3-6 的烯基，等等。